Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Brian F. McGuinness"'
Autor:
Rachael Siegel, Venu Bommireddy, Paget Steven, Albert J. Uveges, Rukiye-Nazan Eraslan, Lee Pellegrino, Krista Saufler, Chia-yu Huang, Eli Mordechai, Haihua Zheng, Gary L. Schieven, Jason Trama, Michael McQueney, Miglena Prabagar, Ku Lu, Axel Metzger, Martin E. Adelson, David Diller, Grant Gallagher, Brian F. Mcguinness, Stanley P. Nawoschik, James R. Beasley
Publikováno v:
Cancer Research. 81:524-524
Introduction: Bacillus Calmette-Guerin (BCG) unresponsive non-muscle invasive bladder cancer (NMIBC) patients are in great need of effective immunotherapies. STING (Stimulator of Interferon Genes) plays a central role in mounting innate and adaptive
Autor:
Xiaolian Xu, Seong Heon Kim, Qingbei Zeng, Joseph A. Kozlowski, Carolyn DiIanni Carroll, Neng-Yang Shih, Baldwin John J, Wensheng Yu, Yueheng Jiang, Guizhen Dong, Yuefei Shao, Brian F. Mcguinness, Gopinadhan N. Anilkumar, Lisa Guise Zawacki, Doug W. Hobbs, Chung-Her Jenh, James W. Hall, Stuart B. Rosenblum, Bandarpalle B. Shankar, De-Yi Yang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6982-6986
The SAR of a novel pyrazinyl-piperazinyl-piperidine scaffold with CXCR3 receptor antagonist activity was explored. Optimization of the DMPK profile and reduction of hERG inhibition is described. Compound 16e with single-digit CXCR3 affinity, good rat
Autor:
W. Lynn Rogers, Brian F. Mcguinness, Kurt W. Saionz, Steven G. Kultgen, Vikash Srivastava, Hema Desai, Hao Yan, Tara M. Stauffer, Samiran Saha, Koc-Kan Ho, Shengting Zhang, Neelima Mannava, Yan Jiang, Anthony E. Klon, Tailong Li, Juxing Yin, Weiqing Chen, Konghua Jing, Maria L. Webb, Kanak Kanti Majumdar, Laura L. Rokosz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7414-7420
A novel series of quinolinone-based adenosine A2B receptor antagonists was identified via high throughput screening of an encoded combinatorial compound collection. Synthesis and assay of a series of analogs highlighted essential structural features
Autor:
Cangming Yang, Biji Jacob-Samuel, Doug W. Hobbs, Joseph A. Kozlowski, Lisa Guise Zawacki, Gopinadhan N. Anilkumar, Guizhen Dong, Carolyn DiIanni Carroll, Brian F. Mcguinness, Stuart B. Rosenblum, Chung-Her Jenh, James W. Hall
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5205-5208
High-throughput screening of an encoded combinatorial aryl piperazine library led to the identification of a novel series of potent piperazinyl-piperidine based CXCR3 antagonists. Analogs of the initial hit were synthesized via solid and solution pha
Autor:
Kenneth J. Valenzano, Kurt W. Saionz, Ruiyan Liu, Dan Xie, Koc-Kan Ho, Edward Mcdonald, Guizhen Dong, Steven G. Kultgen, Peng Geng, Tao Guo, Dan Fitzpatrick, Roland E. Dolle, Anton E.P. Adang, Nicole C.R. van Straten, Brian F. Mcguinness, Maria L. Webb
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1713-1716
High-throughput screening of two million compounds in 37 distinct encoded combinatorial libraries using FSH receptor transfected cells provided small molecule agonists such as 1 (EC50=3 μM) and 2 (EC50=3.9 μM), based on which a focused combinatoria
Autor:
Timothy F. Herpin, Roland E. Dolle, Cullen L. Cavallaro, Yvonne Class Shimshock, Brian F. Mcguinness
Publikováno v:
Tetrahedron Letters. 40:2711-2714
Homoallylic alcohols are prepared in high yield and purity by the reaction of the title reagents with resin-bound aldehydes. The mild reaction conditions accommodate the base-sensitive 4-carboxamido-3-nitrobenzyl photolabile linker on standard resins
Autor:
Brian F. McGuinness, G. William Griffin, George Barany, Christopher Blackburn, Nuria A. Solé, Steven A. Kates, Fernando Albericio
Publikováno v:
Biopolymers. 47:365-380
The choice of a polymeric support is a key factor for the success of solid-phase methods for syntheses of organic compounds and biomolecules such as peptides and oligonucleotides. Classical Merrifield solid-phase peptide synthesis (SPPS), performed o
Autor:
Wong Michael K C, Yueheng Jiang, Qingbei Zeng, Chung-Her Jenh, Stuart B. Rosenblum, De-Yi Yang, Yuefei Shao, Anilkumar G. Nair, Jingqi Duo, Doug W. Hobbs, Brian F. Mcguinness, Joseph A. Kozlowski, Lisa Guise Zawacki, Neng-Yang Shih, Carolyn DiIanni Carroll, Youheng Shu, Seong Heon Kim
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(4)
The structure-human CXCR3 binding affinity relationship of a series of pyridyl/pyrazinyl-piperazinyl-piperidine derivatives were explored with a focus to improve PK, hERG and metabolic profiles. Several small heterocycles were identified as amide sur
Autor:
Mahmoud Aminlari, Thomas Asquith, Katherine Sarlo, Jerome M. Bailey, Oanh Tu, Gilbert Issai, Alice Ha, John E. Shively, Alexander W. Bell, Nicole C. Baur, John J. M. Bergeron, Wei -Jia Ou, David Y. Thomas, Katherine Cianflone, Allain Baldo, Maxwell T. Hincke, Richard L. Momparler, Josée Laliberté, David M. P. Thomson, M. Sutherland, Vladimir Besada, Javier Gonzalez, Gabriel Padron, Hilda Garay, Osvaldo Reyes, Toshifumi Takao, Yasutsugu Shimonishi, Rainer Bischoff, Dominique Roecklin, Bernadette Bouchon, Klaus Klarskov, Alain Van Dorsselaer, Patricia G. Brake, Anne Pacitti, Terry Higgins, Panos Stevis, John Malinowski, Sue McElhiney, Janes Huang, Christine Vestal, Scott D. Buckel, Tracy Stevenson, Joseph A. Loo, Martin Caffrey, Jin Wang, Carmichael J. A. Wallace, Ian Clark-Lewis, C. A. Carothers Carraway, J. Huang, Y. Li, S. -H. Juang, A. Gallo, B. J. Mayer, K. L. Carraway, Patrick L. Coleman, Daniel Sarpong, David W. Deerfield, Amanda Holland-Minkley, John D. Hempel, Hugh B. Nicholas, Nancy D. Denslow, Leroy C. Folmar, Craig V. Sullivan, James D. Dixon, Jonathan P. Mark, Christopher P. Elicone, Simin D. Maleknia, Brian F. McGuinness, Fred E. Regnier, Noubar B. Afeyan, Julia M. Dolence, C. Dale Poulter, Tsezi Egorov, Alexander Musolyamov, Yves Popineau, Jens Andersen, Peter Roepstorff, Roberto J. Falkenstein, Mirtha J. Biscoglio de Jiménez Bonino, Clara Peña, D. L. Gauggel, T. N. Asquith, R. J. Isfort, N. S. Miller, D. B. Cody, Michael F. Giblin, Tuck C. Wong, Thomas P. Quinn, Gregory A. Grant, Mark W. Crankshaw, Scott Griffith, Steve Schroeder, Thomas Quinn, F. Guinet, Y. Petillot, J. M. Chapsal, J. Dubayle, F. Greco, O. Barge, E. Forest, C. Valentin, Frederick M Hahn, Jonathan A. Baker, Mitsuru Haniu, William C. Kenney, Michael F. Rohde, James G. Harman, Eun Ju Lee, Joel Glasgow, Sew Fen Lew, Ali O. Belduz, Reed J. Harris, Michael S. Molony, Lene H. Keyt, Shiaw -Lin Wu, David H. Hawke, Jaqueline Tso, Sherrell Early, Chad G. Miller, G. Thomas Hayman, Jan A. Miernyk, Ulf Hellman, Christer Wernstedt, Jorge Góñez, Daniel Hess, Ralph Studer, Peter E. Hunziker, Hisashi Hirano, Yoshihiro Watanabe, Sergei F. Barbashov, Setsuko Komatsu, Andrew M. Hemmings, Masaru Miyagi, Susumu Tsunasawa, Reuben E. Huber, Nathan J. Roth, Michael T. Gaunt, Paul Jenö, Thierry Mini, Suzette Moes, Martin Horst, Kenji Jinnai, Tetsuo Ashizawa, M. Zouhair Atassi, Anders H. Johnsen, Hanne Jensen, Jens F. Rehfeld, Masaharu Kamo, Takao Kawakami, Norifumi Miyatake, Akira Tsugita, JN Keen, PF Zagalsky, JBC Findlay, Regine Kraft, Susanne Kostka, Enno Hartmann, Henry C. Krutzsch, John K. Inman, Claudia Machalinski, Mirtha Biscoglio de Jiménez Bonino, Donald K. McRorie, Gregg R. Dieckmann, Susan Heilman, William F. DeGrado, Vincent L. Pecoraro, James Kenny, Julie Sahakian, Jacqueline Tso, Mary B. Moyer, William A. Burkhart, Tatyana Muranova, Lubov Makova, Hugh Nicholas, John Hempel, Amy Hinich, David Deerfield, Joseph Behrmann, Alex Ropelewski, Lori Nixon, Leonard Maneri, Kerry Nugent, Ken Stoney, John Wieser, Hiroshi Ohguro, Krzysztof Palczewski, Kenneth A. Walsh, Richard S. Johnson, Leonard C Packman, Carl Webster, John Gray, G. Padrón, V. Morera, L. J. González, Y. Támbara, V. Besada, R. Villalonga, G. Chinea, O. Reyes, H. Garay R. Bringas, C. Nazábal, Bruce P. Parkinson, Kent A. Yamada, Anne Randolph, Anthony Pisano, Nicole H. Packer, John W. Redmond, Keith L. Williams, Andrew A. Gooley, Hanne H. Rasmussen, Ejvind Mørtz, Matthias Mann, Julio E. Celis, Lone K. Rasmussen, Esben S. Sørensen, Torben E. Petersen, Jørgen Gliemann, Poul Henning Jensen, Staffan Renlund, Henrik Wadensten, Annika Persson, Per Persson, Agneta Johansson, Per -Olof Edlund, Donald J. Rose, Ragna Sack, Alex Apffel, Chad Miller, Rodney L. Levine, Kazuyasu Sakaguchi, Nicola Zambrano, Marc S. Lewis, Eric T. Baldwin, Bruce A. Shapiro, John W Erickson, James G. Omichinski, G. Marius Clore, Angela M. Gronenborn, Ettore Appella, Werner Schröder, Irmgard Moser, Werner Pansegrau, Erich Lanka, Richard J. Simpson, James Eddes, Hong Ji, Gavin E. Reid, Robert L. Moritz, Peter Højrup, David W. Speicher, David F. Reim, Kaye D. Speicher, B. R. Srinivasa, S. P. Barde, William G. Stirtan, Alyona Sukhanova, Sergey Vorob'ev, Alexander Gabibov, Igor Bronstein, Kenji Tanaka, Kuniko Einaga, Minoru Tsukada, Jonathan F. Tait, Kazuo Fujikawa, Keiji Takamoto, Kazuo Satake, Ilya A. Vakser, V. V. Velikodvorskaia, A. G. Gabibov, A. G. Rabinkov, Tennie Videler, Michael Osborne, Geoffrey Moore, Richard James, Colin Kleanthous, Jane H. Walent, Richard Bessen, Dick Marsh, Ronald L. Niece, Francis H. C. Tsao, Hong Wang, Scot R. Weinberger, Lynn M. Chakel, Ewald M. Wondrak, Alan R. Kimmel, John M. Louis
Publikováno v:
Journal of Protein Chemistry. 13:515-543
Autor:
Gopinadhan N. Anilkumar, Qingbei Zeng, Brian F. Mcguinness, Chung-Her Jenh, Guizhen Dong, Lisa Guise Zawacki, Inna Schulman, Yueheng Jiang, Seong Heon Kim, Yuefei Shao, Youheng Shu, Wong Michael K C, Doug W. Hobbs, Stuart B. Rosenblum, Neng-Yang Shih, James W. Hall, Carolyn DiIanni Carroll, Wensheng Yu, Joseph A. Kozlowski
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(5)
The structure–human CXCR3 binding affinity relationship of a series of pyridyl–piperazinyl-piperidine derivatives was explored. The optimization campaign highlighted the pronounced effect of 2′-piperazine substitution on CXCR3 receptor affinity